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  • Pharmacological correction of obesity-induced autophagy arrest using calcium channel blockers.

Pharmacological correction of obesity-induced autophagy arrest using calcium channel blockers.

Nature communications (2014-09-06)
Hwan-Woo Park, Haeli Park, Ian A Semple, Insook Jang, Seung-Hyun Ro, Myungjin Kim, Victor A Cazares, Edward L Stuenkel, Jung-Jae Kim, Jeong Sig Kim, Jun Hee Lee
ABSTRACT

Autophagy deregulation during obesity contributes to the pathogenesis of diverse metabolic disorders. However, without understanding the molecular mechanism of obesity interference in autophagy, development of therapeutic strategies for correcting such defects in obese individuals is challenging. Here we show that a chronic increase of the cytosolic calcium concentration in hepatocytes during obesity and lipotoxicity attenuates autophagic flux by preventing the fusion between autophagosomes and lysosomes. As a pharmacological approach to restore cytosolic calcium homeostasis in vivo, we administered the clinically approved calcium channel blocker verapamil to obese mice. Such treatment successfully increases autophagosome-lysosome fusion in liver, preventing accumulation of protein inclusions and lipid droplets and suppressing inflammation and insulin resistance. As calcium channel blockers have been safely used in clinics for the treatment of hypertension for more than 30 years, our results suggest they may be a safe therapeutic option for restoring autophagic flux and treating metabolic pathologies in obese patients.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Rapamycin, Ready Made Solution, 2.5 mg/mL in DMSO (2.74 mM), from Streptomyces hygroscopicus
Supelco
Fumonisin B1 solution, ~50 μg/mL in acetonitrile: water, analytical standard
Sigma-Aldrich
3-[(1R)-1-Hydroxy-2-(methylamino)ethyl]phenol, AldrichCPR
Supelco
Fumonisin B1, reference material, Manufactured by: Sigma-Aldrich Production GmbH, Switzerland
Supelco
Rapamycin, VETRANAL®, analytical standard
Sigma-Aldrich
Monoclonal Anti-α-Tubulin antibody produced in mouse, ascites fluid, clone B-5-1-2
Sigma-Aldrich
L-Cycloserine
Sigma-Aldrich
Fumonisin B1 from Fusarium moniliforme, ≥98% (HPLC)
Sigma-Aldrich
3-Chloro-2-methylphenol, AldrichCPR
Sigma-Aldrich
SP600125, ≥98% (HPLC)
Phenylephrine, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
DAPI, for nucleic acid staining